1. Metabolic Enzyme/Protease
    Apoptosis
  2. Gutathione S-transferase
    Apoptosis
  3. Ezatiostat

Ezatiostat (Synonyms: TER199(free base); TLK199)

Cat. No.: HY-13634A Purity: >96.0%
Handling Instructions

Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment.

For research use only. We do not sell to patients.

Ezatiostat Chemical Structure

Ezatiostat Chemical Structure

CAS No. : 168682-53-9

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10 mM * 1 mL in DMSO USD 112 In-stock
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5 mg USD 96 In-stock
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10 mg USD 162 In-stock
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50 mg USD 480 In-stock
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100 mg USD 816 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment[1][2].

IC50 & Target

Glutathione S-transferase P1-1 (GSTP1)[1]

In Vitro

Ezatiostat causes dissociation of the enzyme from the jun-N-terminal kinase/c-Jun (JNK/JUN) complex, leading to JNK activation by phosphorylation. The therapeutic action of ezatiostat appears to include both proliferation of normal myeloid progenitors as well as apoptosis of the malignant clone[1].
Selection of a resistant clone of an HL60 tumor cell line through chronic exposure to Ezatiostat (TLK199) results in cells with elevated activities of c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2, and allowes the cells to proliferate under stress conditions that induced high levels of apoptosis in the wild type cells[2].

In Vivo

Administration of Ezatiostat (TLK199), stimulates both lymphocyte production and bone marrow progenitor (colony-forming unit-granulocyte macrophage) proliferation, but only in glutathione S-transferase P1-1 (GSTP1+/+) and not in GSTP1-/- animals[2].

Clinical Trial
Molecular Weight

529.65

Formula

C₂₇H₃₅N₃O₆S

CAS No.

168682-53-9

SMILES

O=C(OCC)[[email protected]@H](C1=CC=CC=C1)NC([[email protected]@H](NC(CC[[email protected]](N)C(OCC)=O)=O)CSCC2=CC=CC=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (188.80 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8880 mL 9.4402 mL 18.8804 mL
5 mM 0.3776 mL 1.8880 mL 3.7761 mL
10 mM 0.1888 mL 0.9440 mL 1.8880 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (5.19 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.75 mg/mL (5.19 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (5.19 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

EzatiostatTER199(free base)TLK199TLK 199TLK-199Gutathione S-transferaseApoptosisGlutathione transferasesGSTsMDSGSTP1JNKtripeptideproliferationlymphocyteERK1c-JunInhibitorinhibitorinhibit

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Ezatiostat
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